Siegel J D, McCracken G H, Thomas M L, Threlkeld N
Antimicrob Agents Chemother. 1979 Feb;15(2):246-53. doi: 10.1128/AAC.15.2.246.
Netilmicin and gentamicin susceptibilities of 258 gram-negative organisms and 25 strains of Staphylococcus aureus were nearly identical. The pharmacokinetic properties of netilmicin were evaluated in 101 newborn infants and related to birth weight, gestational age, chronological age, and route of administration. Mean peak serum concentrations of 5.6 to 6.9 and 7.8 to 8.4 mug/ml were observed 30 min after 3- and 4-mg/kg doses, respectively, were given intramuscularly. The peak concentrations were directly related to gestational age. The average serum half-life values varied from 3.4 to 4.7 h and in general were inversely related to birth weight, gestational age, and postnatal age. The pharmacokinetics of netilmicin in 10 infants were similar after intramuscular and intravenous administration. A comparative study of netilmicin and gentamicin in seven neonates revealed greater variability in serum concentrations of gentamicin and a shorter half-life for netilmicin. There was evidence of accumulation of netilmicin in 12 low-birth weight, premature infants who received 4-mg/kg doses for an average of 6.4 days. Serum and urine levels of netilmicin were measured up to 11 days after discontinuation of the drug. These data are well characterized by a two-compartment model. Additional studies of efficacy and long-term toxicity of netilmicin in neonates are necessary.
258株革兰氏阴性菌和25株金黄色葡萄球菌对奈替米星和庆大霉素的敏感性几乎相同。在101名新生儿中评估了奈替米星的药代动力学特性,并将其与出生体重、胎龄、月龄和给药途径相关联。分别肌肉注射3毫克/千克和4毫克/千克剂量后30分钟,观察到平均血清峰值浓度分别为5.6至6.9微克/毫升和7.8至8.4微克/毫升。峰值浓度与胎龄直接相关。平均血清半衰期值在3.4至4.7小时之间变化,总体上与出生体重、胎龄和出生后年龄呈负相关。奈替米星在10名婴儿中肌肉注射和静脉注射后的药代动力学相似。对7名新生儿进行的奈替米星和庆大霉素的比较研究显示,庆大霉素的血清浓度变异性更大,而奈替米星的半衰期更短。有证据表明,12名低出生体重早产儿接受了平均6.4天的4毫克/千克剂量的奈替米星后出现了药物蓄积。在停药后长达11天的时间里测量了奈替米星的血清和尿液水平。这些数据可以用二室模型很好地描述。有必要对奈替米星在新生儿中的疗效和长期毒性进行进一步研究。